OTS186935

Product NameOTS186935
CAS2093400-18-9
MFC25H26ClN5O2
MW463.96
EINECS
MOL File2093400-18-9.mol

Chemical Properties

Density	1.33±0.1 g/cm3(Predicted)
pka	7.32±0.50(Predicted)
form	Solid
color	Off-white to light yellow

Usage And Synthesis

Description

OTS186935 is a protein methyltransferase SUV39H2 inhibitor. OTS186935 shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. It regulates the production of γ-H2AX in cancer cells.

Uses

OTS186935 is a potent protein methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM. OTS186935 shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS193320 regulates the production of γ-H2AX in cancer cells[1].

in vivo

OTS186935 (10 mg/kg or 25 mg/kg; intravenously; once daily for 14 days) exhibits growth suppressive effects in human cancer cell line derived xenograft models^[1].

Animal Model:	Female NOD.CB17-Prkdcscid/J mice (bearing MDA-MB-231 cells )^[1]
Dosage:	10 mg/kg
Administration:	Intravenously; once daily for 14 days
Result:	Tumor growth inhibition of 42.6% on day 14.

Animal Model:	Female BALB/cAJcl-nu/nu mice (bearing A549 cells)^[1]
Dosage:	25 mg/kg
Administration:	Intravenously; once daily for 14 days
Result:	Yielded a tumor growth inhibition of 60.8% without significant body weight loss or toxicity.

References

[1] Vougiouklakis T, et al. Development of novel SUV39H2 inhibitors that exhibit growth suppressive effects in mouse xenograft models and regulate the phosphorylation of H2AX. Oncotarget. 2018 Aug 7;9(61):31820-31831. DOI:10.18632/oncotarget.25806